ChemInform Abstract: Sasanquol, a 3,4-seco-Triterpene Alcohol from Sasanqua Oil, and Its Antiinflammatory Effect.

ChemInform ◽  
2010 ◽  
Vol 29 (39) ◽  
pp. no-no
Author(s):  
T. AKIHISA ◽  
K. YASUKAWA ◽  
Y. KIMURA ◽  
S. YAMANOUCHI ◽  
T. TAMURA
Keyword(s):  
Triterpene Alcohol ◽  
Antiinflammatory Effect

Quantitative relations between structure and antiinflammatory activity of aryloxoalkanoic acids

1988 ◽  
Vol 53 (8) ◽  
pp. 1862-1872 ◽  
Author(s):  
Miroslav Kuchař ◽  
Eva Maturová ◽  
Bohumila Brunová ◽  
Jaroslava Grimová ◽  
Hana Tomková ◽  
...  
Keyword(s):  
Regression Analysis ◽  
Structural Changes ◽  
Antiinflammatory Activity ◽  
Structural Parameters ◽  
Considerable Effect ◽  
Antiinflammatory Effect ◽  
Prolonged Action ◽  
Preclinical Development ◽  
Indicator Variables ◽  
Inhibitory Activities

The antiinflammatory effect of a series of aryloxoalkanoic acids II and of their biphenyl derivatives III was examined by measuring the inhibition of the development of carageenan- and adjuvant-induced edemas. The quantitative relations between the antiinflammatory effect and physicochemical and structural parameters of the compounds tested were evaluated. The equations obtained by the method of regression analysis showed a significant linear dependence of both inhibitory activities on the lipophilicity of the compounds and a considerable effect of some structural changes as expressed by indicator variables. The antiinflammatory effect is especially enhanced in both tests by the presence of a cyclic substituent at the aromatic ring. The high antiinflammatory effect of biphenylyl derivatives III is paralleled by their prolonged action. The prolongation of the effect is most likely a result of a suitable biotransformation of acid III to an efficient metabolite. The structural requirements which resulted from both the regression analysis and from the hypothesis of biotransformation of acids III were utilized in the synthesis of suitably substituted biphenylyloxoalkanoic acids. By this approach derivatives IIIe-i were obtained some of which showed a high antiinflammatory and also protracted effect. 4-(2',4'-Difluorbiphenylyl)-4-oxo-2-methylbutanoic acid (VÚFB-16 066, Flobufen) was chosen for further preclinical development.

2,4-Dihydroxyacetophenone Derivatives as Antileukotrienics with a Multiple Activity Mechanism

1998 ◽  
Vol 63 (1) ◽  
pp. 103-114 ◽  
Author(s):  
Miroslav Kuchař ◽  
Kateřina Čulíková ◽  
Vladimíra Panajotovová ◽  
Bohumila Brunová ◽  
Antonín Jandera ◽  
...  
Keyword(s):  
Significant Inhibition ◽  
Antiinflammatory Effect ◽  
Acid Moiety ◽  
Activity Mechanism

A series of 2,4-dihydroxy-3-propylacetophenone derivatives containing alkylthiobenzoic or arylacetic acid moiety was prepared. The antileukotrienic activity of the substances was assessed in terms of inhibition of the biosynthesis of LTB4 and bonding to LTB4 and LTD4 receptors. Some of the substances were found to exert a complex antileukotrienic effect in all of the three tests. The compounds also displayed an antiinflammatory effect, as manifested by a significant inhibition of LTD4-induced bronchospasm.

scholarly journals Syntheses of two deacetyl-thymosin β4analogs and their anti-inflammatory effect on carrageenin-induced edema in the mouse paw

2001 ◽  
Vol 10 (2) ◽  
pp. 89-92 ◽  
Author(s):  
T. Abiko ◽  
R. Ogawa
Keyword(s):  
Marked Reduction ◽  
Solid Phase ◽  
The Other ◽  
Para Position ◽  
Phase Method ◽  
Antiinflammatory Effect ◽  
Solid Phase Method ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Two {Met(0)6}deacetyl-thymosin β4analogs containing Phe(4F) or Tyr(Me) at position 12 were synthesized by the manual solid-phase method, and their anti-inflammatory effect on carrageenin-induced edema in the mouse paw was studied. Fluorination of the para-position of Phe12resulted in a marked antiinflammatory effect on carrageenin-induced edema in the mouse paw compared with that of our synthetic {Met(0)6}deacetyl-thymosin β4, but the other analog, {Met(0)6, Tyr(Me)12}deacetyl-thymosin β4, showed a marked reduction of the anti-inflammatory effect.

scholarly journals Antiinflammatory effect of androgen receptor activation in human benign prostatic hyperplasia cells

2012 ◽  
Vol 214 (1) ◽  
pp. 31-43 ◽  
Author(s):  
Linda Vignozzi ◽  
Ilaria Cellai ◽  
Raffaella Santi ◽  
Letizia Lombardelli ◽  
Annamaria Morelli ◽  
...  
Keyword(s):  
T Cells ◽  
Growth Factors ◽  
Androgen Receptor ◽  
Benign Prostatic Hyperplasia ◽  
Stromal Cells ◽  
Receptor Activation ◽  
Prostatic Hyperplasia ◽  
Serum Testosterone Level ◽  
Antiinflammatory Effect ◽  
Inflammatory Growth

Progression of benign prostatic hyperplasia (BPH) involves chronic inflammation and immune dysregulation. Preclinical studies have demonstrated that prostate inflammation and tissue remodeling are exacerbated by hypogonadism and prevented by testosterone supplementation. We now investigated whether, in humans, hypogonadism was associated with more severe BPH inflammation and the in vitro effect of the selective androgen receptor agonist dihydrotestosterone (DHT) on cultures of stromal cells derived from BPH patients (hBPH). Histological analysis of inflammatory infiltrates in prostatectomy specimens from a cohort of BPH patients and correlation with serum testosterone level was performed. Even after adjusting for confounding factors, hypogonadism was associated with a fivefold increased risk of intraprostatic inflammation, which was also more severe than that observed in eugonadal BPH patients. Triggering hBPH cells by inflammatory stimuli (tumor necrosis factor α, lipopolysaccharide, or CD4+T cells) induced abundant secretion of inflammatory/growth factors (interleukin 6 (IL6), IL8, and basic fibroblast growth factor (bFGF)). Co-culture of CD4+T cells with hBPH cells induced secretion of Th1 inducer (IL12), Th1-recruiting chemokine (interferon γ inducible protein 10, IP10), and Th2 (IL9)- and Th17 (IL17)-specific cytokines. Pretreatment with DHT inhibited NF-κB activation and suppressed secretion of several inflammatory/growth factors, with the most pronounced effects on IL8, IL6, and bFGF. Reduced inflammatory cytokine production by testosterone cells, an increase in IL10, and a significant reduction of testosterone cells proliferation suggested that DHT exerted a broad antiinflammatory effect on testosterone cells. In conclusion, our data demonstrate that DHT exerts an immune regulatory role on human prostatic stromal cells, inhibiting their potential to actively induce and/or sustain autoimmune and inflammatory responses.

scholarly journals Isolation from Birch Wood of an Aliphatic Oligoterpene Alcohol, a Methyl Ester of Hydroxy-triterpene Carboxylic Acid, and a Triterpene Alcohol.

1964 ◽  
Vol 18 ◽  
pp. 836-837 ◽  
Author(s):  
Bengt O. Lindgren ◽  
E. Kulonen ◽  
K. Sune Larsson ◽  
Hans Halvarson ◽  
Lennart Nilsson
Keyword(s):  
Carboxylic Acid ◽  
Methyl Ester ◽  
Triterpene Alcohol ◽  
Birch Wood
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